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  Immunosuppressant compounds and compositionsUSPTO Application #: 20070203100Title: Immunosuppressant compounds and compositions Abstract: The present invention relates to immunosuppressant, process for their production, their uses and pharmaceutical compositions containing them. The invention provides a novel class of compounds useful in the treatment or prevention of diseases or disorders mediated by lymphocyte interactions, particularly diseases associated with EDG receptor mediated signal transduction. (end of abstract) Agent: Genomics Institute Of The Novartis Research Foundation - San Diego, CA, US Inventors: Shifeng Pan, Thomas H. Marsilje, Wenshuo Lu, Gao Wenqi, Nathanael Schiander Gray, Yun He, Yahua Liu, Yuan Mi, Yongping Xie USPTO Applicaton #: 20070203100 - Class: 514089000 (USPTO) Related Patent Categories: Drug, Bio-affecting And Body Treating Compositions, Designated Organic Active Ingredient Containing (doai), Phosphorus Containing Other Than Solely As Part Of An Inorganic Ion In An Addition Salt Doai, Nitrogen Containing Hetero Ring, Hetero Ring Is Six-membered And Includes Only One Ring Nitrogen The Patent Description & Claims data below is from USPTO Patent Application 20070203100. Brief Patent Description - Full Patent Description - Patent Application Claims
CROSS-REFERENCE TO RELATED APPLICATIONS [0001] This application claims the benefit of priority under 35 U.S.C. .sctn. 119(e) to U.S. Provisional Patent Application No. 60/547,757, filed Feb. 24, 2004. The disclosure of the priority application is incorporated herein by reference in its entirety and for all purposes. BACKGROUND OF THE INVENTION [0002] 1. Field of the Invention [0003] The invention provides a novel class of immunosuppressant compounds useful in the treatment or prevention of diseases or disorders mediated by lymphocyte interactions, particularly diseases associated with EDG receptor mediated signal transduction. [0004] 2. Background [0005] EDG receptors belong to a family of closely related, lipid activated G-protein coupled receptors. EDG-1, EDG-3, EDG-5, EDG-6, and EDG-8 (also respectively termed S1P1, S1P3, S1P2, S1P4, and S1P5) are identified as receptors specific for sphingosine-1-phosphate (S1P). EDG2, EDG4, and EDG7 (also termed LPA1, LPA2, and LPA3, respectively) are receptors specific for lysophosphatidic (LPA). Among the S1P receptor isotypes, EDG-1, EDG-3 and EDG-5 are widely expressed in various tissues, whereas the expression of EDG-6 is confined largely to lymphoid tissues and platelets, and that of EDG-8 to the central nervous system. EDG receptors are responsible for signal transduction and are thought to play an important role in cell processes involving cell development, proliferation, maintenance, migration, differentiation, plasticity and apoptosis. Certain EDG receptors are associated with diseases mediated by lymphocyte interactions, for example, in transplantation rejection, autoimmune diseases, inflammatory diseases, infectious diseases and cancer. An alteration in EDG receptor activity contributes to the pathology and/or symptomology of these diseases. Accordingly, molecules that themselves alter the activity of EDG receptors are useful as therapeutic agents in the treatment of such diseases. SUMMARY OF THE INVENTION [0006] This application relates to compounds of Formula I: [0007] In which: [0008] n is chosen from 0, 1 and 2; m is chosen from 1, 2 and 3; [0009] R.sub.1 is chosen from C.sub.6-10aryl and C.sub.5-10heteroaryl; wherein any aryl or heteroaryl of R.sub.1 is optionally substituted by a radical chosen from C.sub.6-10arylC.sub.0-4alkyl, C.sub.5-6heteroarylC.sub.0-4alkyl, C.sub.3-8cycloalkylC.sub.0-4alkyl, C.sub.3-8heterocycloalkylC.sub.0-4alkyl or C.sub.1-10alkyl; wherein any aryl, heteroaryl, cycloalkyl or heterocycloalkyl group of R.sub.1 can be optionally substituted by 1 to 5 radicals chosen from halo, C.sub.1-10alkyl, C.sub.1-10alkoxy, halo-substituted-C.sub.1-10alkyl and halo-substituted-C.sub.1-10alkoxy; and any alkyl group of R.sub.1 can optionally have a methylene replaced by an atom or group chosen from --S--, --S(O)--, --S(O).sub.2--, --NR.sub.7-- and --O--; wherein R.sub.7 is chosen from hydrogen and C.sub.1-6alkyl; [0010] R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are independently chosen from hydrogen, halo, hydroxy, C.sub.1-10alkyl, C.sub.1-10alkoxy, halo-substituted-C.sub.1-10alkyl and halo-substituted-C.sub.1-10alkoxy; [0011] A is chosen from --X.sub.1C(O)OR.sub.7, --X.sub.1OP(O)(OR.sub.7).sub.2, --X.sub.1P(O)(OR.sub.7).sub.2, --X.sub.1P(O)OR.sub.7, --X.sub.1S(O).sub.2OR.sub.7, --X.sub.1P(O)(R.sub.7)OR.sub.7 and 1H-tetrazol-5-yl; wherein X.sub.1 is chosen from a bond, C.sub.1-3alkylene and C.sub.2-3alkenylene and R.sub.7 is chosen from hydrogen and C.sub.1-6alkyl; [0012] B is CR.sub.8R.sub.9; wherein R.sub.8 and R.sub.9 are independently chosen from hydrogen, hydroxy, C.sub.1-10alkyl, C.sub.1-10alkoxy, halo-substituted-C.sub.1-10alkyl and halo-substituted-C.sub.1-10alkoxy; [0013] E is chosen from CR.sub.8 or N; wherein R.sub.8 is chosen from hydrogen, hydroxy, C.sub.1-10alkyl, C.sub.1-10alkoxy, halo-substituted-C.sub.1-10alkyl and halo-substituted-C.sub.1-10alkoxy; or B is CR.sub.9 and E is carbon and B and E are connected via a double bond; [0014] X is a bond or is chosen from --X.sub.1OX.sub.2--, --X.sub.1NR.sub.7X.sub.2--, --X.sub.1C(O)NR.sub.7X.sub.2--, --X.sub.1NR.sub.7C(O)X.sub.2--, --X.sub.1S(O)X.sub.2--, --X.sub.1S(O).sub.2X.sub.2--, --X.sub.1SX.sub.2--, C.sub.4-6heteroarylene and --X.sub.1ON.dbd.C(R.sub.7)X.sub.2--; wherein X.sub.1 and X.sub.2 are independently chosen from a bond, C.sub.1-3alkylene and C.sub.2-3alkenylene; R.sub.7 is chosen from hydrogen and C.sub.1-6alkyl; and any heteroarylene of X is optionally substituted by a member of the group chosen from halo and C.sub.1-6alkyl; [0015] Y is chosen from C.sub.6-10aryl and C.sub.5-10heteroaryl, wherein any aryl or heteroaryl of Y can be optionally substituted with 1 to 3 radicals chosen from halo, hydoxy, nitro, C.sub.1-10alkyl, C.sub.1-10alkoxy, halo-substituted C.sub.1-10alkyl and halo-substituted C.sub.1-10alkoxy; [0016] and the N-oxide derivatives, prodrug derivatives, protected derivatives, individual isomers and mixtures of isomers thereof; and the pharmaceutically acceptable salts and solvates (e.g. hydrates) of such compounds. [0017] A second aspect of the invention is a pharmaceutical composition which contains a compound of Formula I or an N-oxide derivative, individual isomer or mixture of isomers thereof, or a pharmaceutically acceptable salt thereof, in admixture with one or more suitable excipients. [0018] A third aspect of the invention is a method for treating a disease in an animal in which alteration of EDG receptor mediated signal transduction can prevent, inhibit or ameliorate the pathology and/or symptomology of the disease, which method comprises administering to the animal a therapeutically effective amount of a compound of Formula I or a N-oxide derivative, individual isomer or mixture of isomers thereof; or a pharmaceutically acceptable salt thereof. [0019] A fourth aspect of the invention is the use of a compound of Formula I in the manufacture of a medicament for treating a disease in an animal in which alteration of EDG receptor mediated signal transduction contributes to the pathology and/or symptomology of the disease. [0020] A fifth aspect of the invention is a process for preparing compounds of Formula I and the N-oxide derivatives, prodrug derivatives, protected derivatives, individual isomers and mixtures of isomers thereof; and the pharmaceutically acceptable salts thereof. DESCRIPTION OF THE PREFERRED EMBODIMENTS Continue reading... Full patent description for Immunosuppressant compounds and compositions Brief Patent Description - Full Patent Description - Patent Application Claims Click on the above for other options relating to this Immunosuppressant compounds and compositions patent application. ###  How KEYWORD MONITOR works... a FREE service from FreshPatents1. Sign up (takes 30 seconds). 2. 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